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K 00546

Name: K 00546
Brand: TargetMol
SKU: T21950
Rating: 4.5 (1 reviews)

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Catalog No. T21950Cas No. 443798-47-8

Alias K00546

K 00546 is a potent inhibitor of cellular cyclin kinases (CDK1 and CDK2) and CDC2-like kinases (CLK1 and CLK3) used in the study of cancer and immune-related diseases.

K 00546

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Purity: 99.12%

Catalog No. T21950Alias K00546Cas No. 443798-47-8

K 00546 is a potent inhibitor of cellular cyclin kinases (CDK1 and CDK2) and CDC2-like kinases (CLK1 and CLK3) used in the study of cancer and immune-related diseases.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$98	6-8 weeks	6-8 weeks
5 mg	$265	6-8 weeks	6-8 weeks
25 mg	$920	6-8 weeks	6-8 weeks
50 mg	$1,180	6-8 weeks	6-8 weeks
100 mg	$1,820	6-8 weeks	6-8 weeks
1 mL x 10 mM (in DMSO)	$320	6-8 weeks	6-8 weeks

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.12%

Appearance:Solid

Color:White

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COA

Product Introduction

Bioactivity

Description	K 00546 is a potent inhibitor of cellular cyclin kinases (CDK1 and CDK2) and CDC2-like kinases (CLK1 and CLK3) used in the study of cancer and immune-related diseases.
Targets&IC50	Calmodulin kinase:8.9 μM, CDK2-CyclinA:0.5 nM, GSK-3:0.14 μM, Casein kinase-1:2.8 μM, ERK2:1.0 μM, CLK3:29.2 nM, CDK1-CyclinB:0.6 nM, PKA:5.2 μM, PDGFRβ:1.6 μM, VEGFR2:0.032 μM, CLK1:8.9 nM
In vitro	K 00546 binds to the SLK ATP binding site and forms three hydrogen bonds with the kinase hinge residues E109 and C111. In addition, the aminosulfonyl portion of K 00546 interacts with the backbone of L40. [1] K 00546 also inhibits a number of kinases, including PKA, casein kinase-1, MAP kinase (ERK-2), calmodulin kinase, VEGF-R2, GSK-3, and PDGF-Rβ, with IC50 values of 5.2 μM, 2.8 μM, 1.0 μM, 8.9 μM, 0.032 μM, 0.14 μM, and 1.6 μM, respectively. K 00546 is a potent CDK1 and CDK2 inhibitor with IC50 values of 0.6 nM for CDK1/cyclin B and 0.5 nM for CDK2/cyclin A. [2] K 00546 has also been shown to be a potent CDC2-like kinase 1 (CLK1) and CLK3 inhibitor with IC50 values of 8.9 nM and 29.2 nM, respectively. [3]
Synonyms	K00546

Chemical Properties

Molecular Weight	425.44
Formula	C₁₅H₁₃F₂N₇O₂S₂
Cas No.	443798-47-8
Smiles	O=S(=O)(N)C1=CC=C(C=C1)NC=2N=C(N)N(N2)C(=S)NC=3C(F)=CC=CC3F
Relative Density.	1.72 g/cm3 (Predicted)

Storage & Solubility Information

Storage

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 80 mg/mL (188.04 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3505 mL	11.7525 mL	23.5051 mL	117.5254 mL
5 mM	0.4701 mL	2.3505 mL	4.7010 mL	23.5051 mL
10 mM	0.2351 mL	1.1753 mL	2.3505 mL	11.7525 mL
20 mM	0.1175 mL	0.5876 mL	1.1753 mL	5.8763 mL
50 mM	0.0470 mL	0.2351 mL	0.4701 mL	2.3505 mL
100 mM	0.0235 mL	0.1175 mL	0.2351 mL	1.1753 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc